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Iguratimod (T614; T-614) is a 4H-1-benzopyran-based antirheumatic agent acting as a novel and potent nhibitor of COX-2 (IC50 = 20 μM) with no effect on COX-1. It also inhibits macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM.
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| ln Vitro |
Iguratimod (T-614) is an antirheumatic medication that inhibits COX-2 with an IC50 of 20 μM (7.7 μg/mL) but does not affect COX-1. Iguratimod (0.1–10 μg/mL) reduces bradykinin-induced PGE2 release from fibroblasts. Iguratimod suppresses COX activity in bradykinin-stimulated fibroblasts in a concentration-dependent manner (IC50 = 48 μg/mL). Iguratimod (10 and 30 μg/mL) suppresses COX-2 mRNA in a dose-dependent manner [1]. Furthermore, Iguratimod significantly suppresses macrophage migration inhibitory factor (MIF) with an IC50 of 6.81 μM. In vitro, iguratimod interacts synergistically with glucocorticoids [3].
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| ln Vivo |
In a dose-dependent manner, iguratimod (5 or 20 mg/kg) exhibited analgesic effects and markedly raised the rats' left hindpaw's pain threshold. The rise in pERK1/2 and c-Fos in the spinal cord brought on by cancer cell injection is decreased by iguratimod (5 or 20 mg/kg). In rats, iguratimod similarly decreased IL-6 levels in a dose-dependent manner. Rats treated with Iguratimod have decreased osteoclast activity compared to the control group [2]. It has been demonstrated that iguratimod (20 mg/kg ip) considerably increases the survival of endotoxemia-prone BALB/c mice and reduces isolated TNFα release in the serum of wild-type C57BL/6 mice 90 minutes after LPS injection [3].
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| References |
[1]. Tanaka K, et al. T-614, a novel antirheumatic drug, inhibits both the activity and induction of cyclooxygenase-2 (COX-2) in cultured fibroblasts. Jpn J Pharmacol. 1995 Apr;67(4):305-14.
[2]. Sun Y, et al. Anti-rheumatic drug iguratimod protects against cancer-induced bone pain and bone destruction in a rat model. Oncol Lett. 2017 Jun;13(6):4849-4856. [3]. Iguratimod, et al. Identification of Iguratimod as an Inhibitor of Macrophage Migration Inhibitory Factor (MIF) with Steroid-sparing Potential. J Biol Chem. 2016 Dec 16;291(51):26502-26514 |
| Molecular Formula |
C17H14N2O6S
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| Molecular Weight |
374.37
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| Exact Mass |
374.05726
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| CAS # |
123663-49-0
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| SMILES |
O=CNC1=COC2=C(C=C(OC3=CC=CC=C3)C(NS(=O)(C)=O)=C2)C1=O
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| InChi Key |
ANMATWQYLIFGOK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C17H14N2O6S/c1-26(22,23)19-13-8-15-12(17(21)14(9-24-15)18-10-20)7-16(13)25-11-5-3-2-4-6-11/h2-10,19H,1H3,(H,18,20)
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| Chemical Name |
N-(7-(methylsulfonamido)-4-oxo-6-phenoxy-4H-chromen-3-yl)formamide
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| Synonyms |
T614 T-614 N7methanesulfonamido4oxo6(phenoxy)chromen3ylformamide
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~89.03 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (6.68 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6712 mL | 13.3558 mL | 26.7115 mL | |
| 5 mM | 0.5342 mL | 2.6712 mL | 5.3423 mL | |
| 10 mM | 0.2671 mL | 1.3356 mL | 2.6712 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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